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GLP-1 receptor stimulation preserves primary cortical and dopaminergic neurons in cellular and rodent models of stroke and Parkinsonism
TLDR
It is demonstrated that Ex-4 can protect neurons against metabolic and oxidative insults, and they provide preclinical support for the therapeutic potential for exendin-4 in the treatment of stroke and PD.
Selective butyrylcholinesterase inhibition elevates brain acetylcholine, augments learning and lowers Alzheimer beta-amyloid peptide in rodent.
TLDR
In rats, cymserine analogs caused long-term inhibition of brain BChE and elevated extracellular ACh levels, without inhibitory effects on acetylcholinesterase, and improved the cognitive performance of aged rats.
Phenserine regulates translation of β-amyloid precursor protein mRNA by a putative interleukin-1 responsive element, a target for drug development
TLDR
It is suggested that phenserine reduces Aβ levels by regulating βAPP translation via the recently described iron regulatory element in the 5′-untranslated region of βAPP mRNA, which has been shown previously to be up-regulated in the presence of interleukin-1.
Presence and formation of codeine and morphine in the rat.
TLDR
To demonstrate occurrence of a biosynthetic pathway to morphine in mammals similar to that used by the poppy plant, (+)-salutaridine, (-)-thebaine, and (-)-codeine were administered to rats intravenously and caused a marked increase in the codeine and morphine levels in rat tissues.
Studies in the (+)-morphinan series. 5. Synthesis and biological properties of (+)-naloxone.
TLDR
(+)-Naloxone was prepared in 26% overall yield in eight steps from (+)-7-bromodihydrocodeinone dimethyl ketal by a synthesis which excluded enantiomeric contamination, and can serve to test the stereospecificity of the biochemical and pharmacological actions of (-)-nalox one.
Comparative inhibitory effects of various physostigmine analogs against acetyl- and butyrylcholinesterases.
TLDR
Results do show that the structure of physostigmine can be changed significantly while retaining biological activity and the phenyl substitution appears to increase greatly the selectivity of the compound for AChE.
Arteether, a new antimalarial drug: synthesis and antimalarial properties.
TLDR
Crystalline arteether and its oily epimer 7 were 2-3 times more potent schizontocides than quinghaosu (1), but deoxy compounds 8, 9, and 11 were 100-300 times less potent in vitro than their corresponding peroxy precursors.
Inhibition of monoamine oxidases A and B by simple isoquinoline alkaloids: racemic and optically active 1,2,3,4-tetrahydro-, 3,4-dihydro-, and fully aromatic isoquinolines.
TLDR
The concept that the topography of the inhibitor binding site differs in MAO A and B is supported.
Mapping the binding site of colchicinoids on beta -tubulin. 2-Chloroacetyl-2-demethylthiocolchicine covalently reacts predominantly with cysteine 239 and secondarily with cysteine 354.
TLDR
A significant conformational change must occur in the colchicine binding site of tubulin in the transition from the unpolymerized to the polymerized state.
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